Ranolazine (hydrochloride)

Ranolazine is a piperazine derivative with cardioprotective activity. It reduces the late sodium current (INa) in mouse myocytes expressing the long QT syndrome 3 mutant sodium channel DKPQ, ventricular myocytes isolated from a canine model of heart failure, guinea pig ventricular myocytes exposed to hydrogen peroxide or anemone toxin-II, and HEK293 cells expressing human Nav1.5 channels (IC50s = 5.9-15 µM) as well as the late potassium current (IKr) in canine ventricular myocytes and HEK293 cells (IC50s = 11.5 and 14.4 µM, respectively). Ranolazine also inhibits radioligand binding to alpha1-, beta1-, and beta2-adrenergic receptors (Kis = 8.2-19.5, 1.4-8.6, and 0.5-14.8 µM, respectively). In vivo, ranolazine (480 µg/kg per min) reduces clofilium-induced prolongation of the QTc interval and Torsade de Pointes (TdP) in rabbits. Ranolazine also reduces interstitial collagen deposition as well as atrial natriuretic peptide (ANP, Cay-24539, Cay-24276), connective tissue growth factor (CTGF), brain natriuretic peptide (BNP, Cay-24541), and matrix metalloproteinase-2 (MMP-2) mRNA levels, and prevents left ventricular dilation in a mouse model of cardiotoxicity induced by doxorubicin (Cay-15007).Formal Name: N-(2,6-dimethylphenyl)-4-[2-hydroxy-3-(2-methoxyphenoxy)propyl]-1-piperazineacetamide, dihydrochloride. CAS Number: 95635-56-6. Synonyms: RS 43285. Molecular Formula: C24H33N3O4 . 2HCl. Formula Weight: 500.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 20 mg/ml, PBS (pH 7.2): 10 mg/ml. lambdamax: 272 nm. SMILES: OC(COC1=C(OC)C=CC=C1)CN2CCN(CC(NC3=C(C)C=CC=C3C)=O)CC2.Cl.Cl. InChi Code: InChI=1S/C24H33N3O4.2ClH/c1-18-7-6-8-19(2)24(18)25-23(29)16-27-13-11-26(12-14-27)15-20(28)17-31-22-10-5-4-9-21(22)30-3,,/h4-10,20,28H,11-17H2,1-3H3,(H,25,29),2*1H. InChi Key: RJNSNFZXAZXOFX-UHFFFAOYSA-N.